FUROPYRIDINES AS BROMODOMAIN INHIBITORS Russian patent published in 2018 - IPC C07D491/48 A61K31/34 A61K31/4355 A61K31/5025 A61P29/00 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel furopyridine derivatives of formula I

where: V is N or C-R₂; W is N or C-R₈; X is N, CH or C(CH₃); Y is N or C-R₅; Z is N or C-R₁₅; Q is N or CH; R₁ is C_1-4alkyl or deuterated C_1-4alkyl; R₂, when present, is H, OH, -NH₂, -OC_1-4alkyl, -NHC(O)H, -NHC(O)C_1-4alkyl, -H(CH₃)C(O)C_1-4alkyl, -NHC(O)NH₂, -NHC(O)C_1-4alkyleneNH₂, -N(CH₃)C(O)NH₂, -N(CH₃)C(O)C_1-4alkyleneNH₂, -OC_2-4alkyleneOCH₃, -OC_2-4alkyleneOH or R₂ is a group selected from -G-CH₂CH(R₃)(R₄), -G-CH(R₃)(R₄) and -G-R₃, in which G is NH, N(CH₃), O, C(O)NH or NHC(O); R₃ is phenyl, pyridinyl, C_3-7cycloalkyl or a 5-6 membered heterocycle containing an oxygen or nitrogen atom and optionally substituted with =O; and R₄ is H or C_1-4alkyl; R₅, when present, is H, OH, -OC_1-4 alkyl, -CH₂NH₂, -OCF₃, -C(O)NHC_1-4alkyl or -CO₂H; R₆ is -NR₁₁R₁₂ or group

D is CH or N; E is N, O, CH or SO₂; R₇, when present, is H, OH, C_1-4 alkyl, -SO₂C_1-4alkyl, -NHSO₂CH₃, -C(O)C_1-4alkyl; R₈, when present, is H, C_1-4 alkyl, OH, -OC_1-4 alkyl, -OC_2-4alkyleneOC_1-4 alkyl, -OCF_3; -OC_1-4alkyleneF, -OC_1-4alkyleneCHF₂, -OC_2-4alkyleneOH, -Ophenyl, -OC_1-4alkylenephenyl, -NHC_3-7cycloalkyl, -NHC_1-4alkylene C_3-7cycloalkyl, -OC_3-7cycloalkyl, -OC_1-4alkyleneC_3-7cycloalkyl, -NHC_4-6heterocycle, -NHC_1-4alkyleneC_4-6heterocycle, -OC_4-6heterocycle or -OC_1-4alkylene C_4-6heterocycle, containing as a heteroatom N or O, where each C_3-7cycloalkyl or C_4-6heterocycle is optionally substituted with one or two substituents independently selected from halogen and oxo; or R₈ and R₂ together with the carbon atoms to which they are attached form a heterocycle containing as a heteroatom N and optionally substituted oxo; R₉ is H, C_1-4alkyl, halogen, OH, -OC_1-4alkyl, -CH₂OH, -C(O)NHCH₃, -C(O)NH(CH₃)₂; R₁₀ is H, C_1-4alkyl, halogen, OH, -OC_1-4alkyl or oxo; R₁₁ is H, C_1-4alkyl or SO₂CH₃; R₁₂ is H, C_1-4alkyl, C_2-4alkyleneNHR₁₃, SO₂CH₃, a 5-6 membered heterocycle containing SO₂; R₁₃ is H or SO₂CH₃; R₁₄ is H or C_1-4alkyl; R₁₅ is H, C_1-4alkyl or NHC(O)C_1-4alkyl; R₁₆ is H or C_1-4alkyl; and each of n and m is an integer independently selected from 0, 1 and 2; provided that no more than 2 of V, W, X, Y and Z are N; or salts thereof.

EFFECT: invention also relates to a pharmaceutical composition having bromodomain inhibitor activity, based on said compounds, use thereof in the manufacture of a medicament for use in the treatment of diseases or conditions, for which a bromodomain inhibitor is indicated, and a method of treating such diseases or conditions.

18 cl, 2 tbl, 109 ex